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Nicotinic acetylcholine receptor (nAChR) agonists, antagonists and modulators act on ligand-gated cation channels. Each receptor is a pentamer of subunits arranged around a central pore that opens when acetylcholine binds. A refined structure of the Torpedo receptor at 4 Å resolution, published in 2005, resolved its ligand-binding, membrane and cytoplasmic regions. Muscle-type receptors mediate neuromuscular transmission, while neuronal subtypes such as α7 and α4β2 are studied in attention, memory and nicotine dependence. Agonists include PNU 282987, which is selective for α7, and the partial agonist varenicline. PNU-120596, described in 2005, is a positive allosteric modulator of α7 that enhances acetylcholine-evoked currents. Vecuronium bromide, a neuromuscular blocking agent, acts on the muscle-type receptor.
Synonyms: S169611
S16961 is a potent agonist of nicotinic acetylcholine receptors (nAChRs). This compound induces receptor activation, making it valuable for studies related to neurotransmission and synaptic plasticity. Research applications include exploring neurological disorders, cognitive function, and the mechanisms of addiction.
NS3861 fumarate is a potent agonist of the heteromeric α3β4 nicotinic acetylcholine receptor (nAChR), exhibiting high affinity with a binding Ki of 0.62 nM. This compound selectively engages with α3β4 nAChRs while also demonstrating varying affinities for other nAChR subtypes, including α3β2 (25 nM), α4β4 (7.8 nM), and α4β2 (55 nM). NS3861 fumarate is primarily used in neurological research to investigate nAChR functions and their roles in neuropharmacology.
Synonyms: WAY-317538
SEN12333 is a potent and selective agonist of the α7 nicotinic acetylcholine receptor (nAChR). It demonstrates high affinity for rat α7 nAChRs, with a Ki value of 260 nM, and functions as a full agonist in calcium flux studies, achieving an EC50 of 1.6 μM. This compound is utilized in research focusing on Alzheimer's disease and schizophrenia, facilitating the exploration of therapeutic interventions targeting cholinergic signaling pathways.
(Rac)-ABT-202 dihydrochloride is a racemic mixture that functions as an agonist for nicotinic acetylcholine receptors (nAChRs). This compound exhibits notable analgesic properties, making it useful in pain research. Its action on nAChRs elucidates potential pathways in neurological studies and could contribute to the development of novel pain management therapies.
Epiboxidine hydrochloride is a potent and selective agonist of the nicotinic acetylcholine receptors (nAChRs), exhibiting Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. This compound, a methylisoxazole analog of the alkaloid Epibatidine, plays a critical role in studying nAChR-mediated signaling pathways. Its high affinity and selectivity make it valuable for research applications in neurobiology and pharmacology, particularly in the exploration of neurological disorders and drug development targeting nAChRs.
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SIB-1553A is a selective agonist of nicotinic acetylcholine receptors (nAChRs), specifically targeting β4 subunit-containing receptors. This compound exhibits neuroprotective properties and enhances cognitive function, making it a valuable tool in the study of Alzheimer’s disease and other cognitive disorders. Its oral bioavailability further supports its potential for therapeutic applications in cognitive enhancement.
(±)-Anatoxin A fumarate is a potent agonist of nicotinic receptors, specifically engaging α4β2 and α7 subtypes with Ki values of 1.25 nM and 1.84 μM, respectively. This compound effectively stimulates [3H]-dopamine release in rat striatal synaptosomes, demonstrating an EC50 of 134 nM. Its biological activity makes it a valuable tool for studying neurotransmitter release and nicotinic receptor function, while also highlighting its toxic effects on aquatic organisms.
Synonyms: d-Epibatidine
Epibatidine dihydrochloride is a potent agonist of nicotinic acetylcholine receptors (nAChRs), significantly influencing neurotransmission and synaptic activity. Its strong affinity for nAChRs makes it a valuable tool for studying cholinergic signaling pathways and their implications in various neurological disorders. This compound is commonly utilized in research aimed at elucidating the roles of nAChRs in addiction, pain modulation, and cognitive functions.
(E/Z)-Acetamiprid is a neonicotinoid insecticide acting as an agonist of nicotinic acetylcholine receptors (nAChR). Its mechanism of action involves the modulation of neurotransmission, which is critical in neuromuscular junction function. This compound is primarily utilized in research exploring insect physiology, neurobiology, and the potential effects of insecticides on reproduction and neuromuscular disorders.
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PHA-543613 hydrochloride is a potent agonist of the α7 nicotinic acetylcholine receptor (nAChR) with demonstrated brain permeability. This compound selectively targets α3β4, α1β1γδ, α4β2, and 5-HT3 receptors. PHA-543613 hydrochloride has shown significant effects on sensory gating and memory in in vivo models of schizophrenia, making it valuable for research in neuropharmacology and psychopharmacology.
PHA-543613 dihydrochloride is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR), exhibiting a Ki value of 8.8 nM. This compound is orally active and capable of penetrating the blood-brain barrier, making it suitable for in vivo studies. PHA-543613 dihydrochloride demonstrates strong selectivity for the α7 nAChR over α3β4, α1β1γδ, α4β2, and 5-HT3 receptors. It is applied in research pertinent to cognitive deficits associated with Alzheimer's disease and schizophrenia.
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DBO-83 dihydrochloride is an innovative agonist of the nicotinic acetylcholine receptor (nAChR), exhibiting a high affinity for nAChRs in rat cortical membranes with a Ki value of 4.1 nM. This compound demonstrates significant antinociceptive and anti-amnesic properties, making it a valuable tool for research into pain modulation and cognitive function. Its potential applications in neuroscience and pharmacology make DBO-83 dihydrochloride a critical reagent for studying neuronal signaling pathways and associated disorders.
Synonyms: α-Lobeline sulfate; L-Lobeline sulfate
Lobeline sulfate is a potent nicotinic receptor agonist known for its ability to penetrate the blood-brain barrier. It enhances dopamine release by inhibiting dopamine uptake into synaptic vesicles and modifying presynaptic dopamine storage. This compound has demonstrated efficacy in supporting smoking cessation efforts, making it a valuable tool for research in addiction and neuropharmacology.
A85380 is a high-affinity agonist for neuronal nicotinic acetylcholine receptors (nAChRs), demonstrating selectivity for the α4β2 nAChR subtype. This compound has been shown to possess a broad-spectrum analgesic profile, making it valuable in pain research. Its distinct mechanism of action offers potential insights into the therapeutic applications of nAChR modulation in various neurological disorders.
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nAChR agonist 2 is a selective agonist for the α4β2 nicotinic acetylcholine receptor (nAChR) with a dissociation constant (Kd) of 26 nM. This compound demonstrates significant biological activity in modulating neurotransmitter release and enhancing synaptic transmission. It is valuable for research applications involving neuropharmacology and the study of neurological disorders associated with cholinergic signaling.
RJR-2429 dihydrochloride is an agonist of the α4β2 and α7 nicotinic acetylcholine receptors (nAChRs). This compound exhibits significant biological activity in modulating neurotransmission and is widely used in research to explore the role of nAChRs in neuronal signaling, cognitive processes, and neurodegenerative diseases. Its selective action on these receptor subtypes makes it a valuable tool for investigating cholinergic pathways and their implications in various physiological and pathological conditions.
Synonyms: AZD1446
TC-6683 is a selective agonist of the α4β2 nicotinic acetylcholine receptor (nAChR). This compound has shown potential in modulating cholinergic signaling pathways and is primarily utilized in research related to neurological disorders, particularly cognitive dysfunction. Although TC-6683 demonstrated limited therapeutic efficacy in an animal model of DYT1 dystonia, its role in studying nAChR dynamics makes it a valuable tool for investigating various neurobiological processes.
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TC299423 is a selective and potent agonist of the α6β2 and α4β2 nicotinic acetylcholine receptors (nAChRs) with significant anxiolytic and antinociceptive properties. This orally active compound effectively penetrates the blood-brain barrier and primarily targets the α6β2 nAChRs, which are associated with the anxiolytic effects of nicotine. Research indicates that TC299423 induces reward-related behaviors in α6L90’S hypersensitive mice and stimulates dopamine release without inhibiting nicotine self-administration in rats. Its pharmacological profile suggests potential applications in the study of addiction and Parkinson's disease.
PHA 568487 is a selective agonist of the α-7 nicotinic acetylcholine receptor (α-7 nAchR). This compound demonstrates significant biological activity in reducing neuroinflammation and oxidative stress, making it valuable for research in neurodegenerative diseases and cognitive disorders. Its ability to rapidly penetrate the blood-brain barrier enhances its potential for therapeutic applications in central nervous system studies.
A 844606 is a highly selective agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), demonstrating potent activation of this target. Its significant biological activity makes it a valuable tool for investigating neurodegenerative and psychiatric conditions, including schizophrenia, Huntington's disease, Alzheimer's disease, and Parkinson's disease. Researchers can utilize A 844606 to explore the role of α4β2 nAChR in these disorders and to assess potential therapeutic strategies.
Synonyms: (S)-Anabasine hydrochloride; (+)-Anabasine hydrochloride
Anabasine hydrochloride is a potent agonist of nicotinic acetylcholine receptors (nAChRs). This alkaloid, derived from tobacco (Nicotiana), functions as a full agonist, inducing depolarization in TE671 cells that endogenously express human fetal muscle-type nAChRs (EC50 = 0.7 µM). Anabasine hydrochloride is relevant for research applications in neurobiology and toxicology, particularly in studies exploring nAChR signaling and muscle contraction mechanisms.
SEN 78702 is an orally active, selective full agonist of the α7 nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.13. This compound is known to enhance memory functions, making it a valuable tool for research in cognitive disorders. Additionally, SEN 78702 exhibits an acceptable level of hERG inhibition (IC50: 15.8 μM), indicating its potential for further pharmacological investigations.
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Synonyms: α-Lobeline; L-Lobeline
Lobeline is a potent nicotinic acetylcholine receptor (nAChR) agonist that effectively penetrates the blood-brain barrier. By inhibiting dopamine (DA) uptake into synaptic vesicles and altering presynaptic DA storage, Lobeline enhances DA release. It is primarily utilized in research focused on addiction and smoking cessation, making it a valuable reagent in the study of dopaminergic signaling pathways.
Epiboxidine is a potent and selective agonist of neural nicotinic acetylcholine receptors (nAChRs), demonstrating Ki values of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. As a methylisoxazole derivative of the alkaloid Epibatidine, Epiboxidine serves as a valuable tool for studying nAChR-related pathways and their physiological functions. This compound is instrumental in exploring the potential therapeutic applications in neuropharmacology and other related fields.
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Synonyms: RJR-2403 fumarate; (E)-Metanicotine fumarate
Rivanicline fumarate is a selective agonist of neuronal nicotinic acetylcholine receptors (nAChRs), primarily targeting the α4β2 subtype with a Ki of 26 nM and an EC50 of 16 μM. This compound has demonstrated the ability to significantly restore learning impairments and alleviate cognitive dysfunctions. Rivanicline fumarate is valuable in research focused on neurodegenerative diseases, including schizophrenia and Alzheimer's disease, providing insights into potential therapeutic approaches.
